Engineered Cyclotides with Potent Broad in Vitro and in Vivo Antimicrobial Activity

Autor:	Teshome Leta Aboye, Lisa Ramirez, Rajasekaran Ganesan, Julio A. Camarero, Paul M. Beringer, Steven Beringer, Mansour A. Dughbaj, Alexander Shekhtman
Rok vydání:	2021
Předmět:	medicine.drug_class Chemistry Organic Chemistry Antibiotics Cyclotides General Chemistry Drug resistance Microbial Sensitivity Tests Antimicrobial medicine.disease Catalysis In vitro Article Cyclotide Microbiology Anti-Bacterial Agents Mice Anti-Infective Agents In vivo Bacteremia Pseudomonas aeruginosa medicine Animals Humans Antibacterial activity
Zdroj:	Chemistry
ISSN:	1521-3765
Popis:	The search for novel antimicrobial agents to combat microbial pathogens is intensifying in response to the rapid development of drug resistance to current antibiotic therapeutics. Respiratory failure and septicemia are the leading causes of mortality among hospitalized patients. Here, the development of a novel engineered cyclotide with effective broad-spectrum antibacterial activity against several ESKAPE bacterial strains and clinical isolates is reported. The most active antibacterial cyclotide was extremely stable in serum, showed little hemolytic activity, and provided protection in vivo in a murine model of P. aeruginosa peritonitis. These results highlight the potential of the cyclotide scaffold for the development of novel antimicrobial therapeutic leads for the treatment of bacteremia.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e8e7ec2436b33da9a515de8663c9e68 https://pubmed.ncbi.nlm.nih.gov/34159664 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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